SN2 Ring Opening of β-Lactones: An Alternative to Catalytic Asymmetric Conjugate Additions

Abstract
Merging catalytic asymmetric acyl halide-aldehyde cyclocondensation (AAC) reactions with ensuing Grignard-mediated ring opening of the derived enantiomerically enriched β-lactones is presented as a generally useful asymmetric synthesis of β-disubstituted carboxylic acids. Enantiomerically enriched β-lactones are subject to efficient SN2 ring opening with a variety of copper-modified alkyl Grignard reagents, including highly branched nucleophiles. Considerable structural variation in the lactone electrophile is also tolerated. Phenyl- and vinyl-derived organometallics are not efficient nucleophiles for the ring-opening reactions.

This publication has 21 references indexed in Scilit: